| Identification | Back Directory | [Name]
Benzamide, 4-[[(3-acetylphenyl)amino]sulfonyl]-N-[4-(3-fluorophenyl)-2-thiazolyl]- | [CAS]
2893778-31-7 | [Synonyms]
PHGDH-IN-3
Benzamide, 4-[[(3-acetylphenyl)amino]sulfonyl]-N-[4-(3-fluorophenyl)-2-thiazolyl]- | [Molecular Formula]
C24H18FN3O4S2 | [MOL File]
2893778-31-7.mol | [Molecular Weight]
495.55 |
| Hazard Information | Back Directory | [Uses]
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer[1]. | [in vivo]
PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) exhibits excellent in vivo pharmacokinetic properties[1].
PHGDH-IN-3 (i.p.; 12.5, 25, 50 mg/kg; once daily for consecutive 31 days) exertes evident antitumor efficacy in the PC9 xenograft mouse model[1]. | Animal Model: | ICR mice[1] | | Dosage: | 1, 3 mg/kg | | Administration: | Oral (p.o.) and intravenous (i.v.) administration | | Result: | | PK parameters | i.v. (1 mg/kg) | p.o. (3 mg/kg) | | AUC (h?ng/mL) | 38,358 ± 14,768 | 94,386 ± 23,416 | | T1/2(h) | 4.94 ± 0.38 | 4.74 ± 0.30 | | Tmax (h) | | 3.33 ± 1.15 | | CL_obs(mL/min/kg) | 0.48 ± 0.23 | | | Cmax(ng/mL) | | 8842 ± 1755 | | F (%) | | 82.0 |
|
| Animal Model: | Balb/c nude mice[1] | | Dosage: | 12.5, 25, 50 mg/kg | | Administration: | Intraperitoneal (i.p.); once daily for consecutive 31 days | | Result: | Exhibited an in vivo anti-tumor effect and significantly delayed the tumor growth.
Significantly abated the tumor weights of mice at 25 mg/ kg.
|
| [References]
[1] Dingding Gao, et al. Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy. J Med Chem. 2023 Jan 12;66(1):285-305. DOI:10.1021/acs.jmedchem.2c01202 |
|
|